U.S. patent application number 13/689947 was filed with the patent office on 2013-06-13 for administration of coumarin, butylated hydroxyanisole and ethoxyquine for the treatment of canities.
This patent application is currently assigned to L'OREAL. The applicant listed for this patent is Stephane COMMO. Invention is credited to Stephane COMMO.
Application Number | 20130149360 13/689947 |
Document ID | / |
Family ID | 37969968 |
Filed Date | 2013-06-13 |
United States Patent
Application |
20130149360 |
Kind Code |
A1 |
COMMO; Stephane |
June 13, 2013 |
ADMINISTRATION OF COUMARIN, BUTYLATED HYDROXYANISOLE AND
ETHOXYQUINE FOR THE TREATMENT OF CANITIES
Abstract
At least one compound selected from among coumarin and/or
derivative thereof, butylated hydroxyanisole, ethoxyquine and
mixtures thereof, and admixtures thereof with other active agents
selected from among active agents for combating desquamative
conditions of the scalp, plant extracts having propigmenting
activity and active agents that slow hair loss and/or promote hair
regrowth, are useful for preventing and/or limiting and/or stopping
the development of canities.
Inventors: |
COMMO; Stephane; (Chaville,
FR) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
COMMO; Stephane |
Chaville |
|
FR |
|
|
Assignee: |
L'OREAL
Paris
FR
|
Family ID: |
37969968 |
Appl. No.: |
13/689947 |
Filed: |
November 30, 2012 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
11812571 |
Jun 20, 2007 |
8344021 |
|
|
13689947 |
|
|
|
|
60819399 |
Jul 10, 2006 |
|
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Current U.S.
Class: |
424/401 ;
424/70.1; 424/74 |
Current CPC
Class: |
A61P 17/14 20180101;
A61Q 5/00 20130101; H01L 2924/0002 20130101; A61K 8/498 20130101;
A61P 17/00 20180101; H01L 2924/0002 20130101; A61Q 5/065 20130101;
A61K 8/347 20130101; A61K 8/4926 20130101; H01L 2924/00
20130101 |
Class at
Publication: |
424/401 ;
424/70.1; 424/74 |
International
Class: |
A61K 8/49 20060101
A61K008/49; A61K 8/34 20060101 A61K008/34; A61Q 5/00 20060101
A61Q005/00 |
Foreign Application Data
Date |
Code |
Application Number |
Jun 20, 2006 |
FR |
0652556 |
Claims
1. -5. (canceled)
6. A cosmetic composition useful for preventing and/or limiting
and/or stopping the development of canities in a subject in need of
such treatment, comprising a thus effective amount of admixture of
coumarin and/or derivatives thereof, butylated hydroxyanisole and
ethoxyquine, formulated into a cosmetically acceptable medium
therefor.
7. A cosmetic composition useful for preventing and/or limiting
and/or stopping the development of canities in a subject in need of
such treatment, comprising a thus effective amount of admixture of
at least one compound selected from the group consisting of
coumarin and derivatives thereof, butylated hydroxyanisole,
ethoxyquine and mixture thereof, and at least one other active
agent selected from the group consisting of active agents for
combating desquamative conditions of the scalp, plant extracts
having propigmenting activity and mixtures thereof, formulated into
a cosmetically acceptable medium therefor.
8. A cosmetic composition useful for preventing and/or limiting
and/or stopping the development of canities in a subject in need of
such treatment, comprising a thus effective amount of admixture of
at least one compound selected from the group consisting of
coumarin and derivatives thereof, butylated hydroxyanisole,
ethoxyquine and mixture thereof, and at least one other active
agent selected from the group consisting of active agents that slow
hair loss, promote hair regrowth and mixtures thereof, formulated
into a cosmetically acceptable medium therefor.
9. The cosmetic composition as defined by claim 7, said at least
one compound being encapsulated in a coating of microspheres,
nanospheres, oleosomes or nanocapsules.
10. The cosmetic composition as defined by claim 8, said at least
one compound being encapsulated in a coating of microspheres,
nanospheres, oleosomes or nanocapsules.
11. The cosmetic composition as defined by claim 7, formulated into
a topically applicable, cosmetically acceptable medium
therefor.
12. The cosmetic composition as defined by claim 8, formulated into
a topically applicable, cosmetically acceptable medium
therefor.
13. The cosmetic composition according to claim 7 or claim 8,
wherein said coumarin and derivatives thereof, butylated
hydroxyanisole, ethoxyquine and mixture thereof is present in an
amount from 0.001% to 10% by weight relative to the total weight of
the composition.
14. The cosmetic composition according to claim 7 or claim 8,
wherein said composition is administered orally, topically to the
skin, topically to any cutaneous area covered with hair, and/or
topically to the scalp.
15. The cosmetic composition according to claim 7 or claim 8,
wherein said compound is contained in a vesicle whose diameter is
less than or equal to 10 .mu.m.
Description
CROSS-REFERENCE TO PRIORITY/PROVISIONAL APPLICATIONS
[0001] This application claims priority under 35 U.S.C. .sctn.119
of FR 0652556, filed Jun. 20, 2006, and of U.S. Provisional
Application No. 60/819,399, Jul. 10, 2006, each hereby expressly
incorporated by reference in its entirety and each assigned to the
assignee hereof.
BACKGROUND OF THE INVENTION
[0002] 1. Technical Field of the Invention
[0003] The present invention relates to the cosmetic administration
of coumarin and derivatives thereof, butylated hydroxyanisole and
ethoxyquine for treating canities.
[0004] 2. Description of Background and/or Related and/or Prior
Art
[0005] The hair follicle is a tubular invagination of the epidermis
which extends to the deep layers of the dermis. The lower part, or
hair bulb, itself comprises an invagination in which the dermal
papilla is located. The lower part of the bulb is an area of cell
proliferation where the precursors of the keratinized cells that
form hair are found. The ascending cells derived from these
precursors become gradually keratinized in the upper part of the
bulb, and this assembly of keratinized cells will form the hair
shaft.
[0006] The color of head hair and of body hair depends especially
on the presence, in variable amounts and ratios, of two groups of
melanins: eumelanins (brown and black pigments) and pheomelanins
(red and yellow pigments). The pigmentation of head hair and body
hair requires the presence of melanocytes in the bulb of the hair
follicle. These melanocytes are in an active state, that is to say
that they synthesize melanins. These pigments are transmitted to
the keratinocytes intended to form the hair shaft, which will
result in the growth of a pigmented head hair or body hair. This
structure is hereinafter called "follicular pigmentation unit".
[0007] In mammals, melanogenesis involves at least three enzymes:
tyrosinase, DOPAchrome tautomerase (TRP-2, for Tyronsinase Related
Protein 2) and DHICAoxidase (TRP-1, for Tyrosinase Related Protein
1).
[0008] Tyrosinase is the enzyme that initiates the biosynthesis of
melanins. It is also described as being the limiting enzyme of
melanogenesis.
[0009] TRP-2 catalyzes the tautomerization of DOPAchrome to
5,6-dihydroxyindole-2-carboxylic acid (DHICA). In the absence of
TRP-2, the DOPAchrome undergoes a spontaneous decarboxylation to
form 5,6-dihydroxyindole (DHI).
[0010] DHICA and DHI are both pigment precursors, TRP-1 oxidizes
DHICA molecules to form quinine derivatives (Pawelek, J. M. and
Chakraborty A. K., "The enzymology of melanogenesis" in "The
Pigmentary System: Physiology and Pathophysiology", by Nordlund, J.
J., Boissy, R. E., Hearing, V. J., King, R. A., Ortonne, J-P., New
York, Oxford University Press, 1998, p. 391-400).
[0011] The three enzymes, tyrosinase, TRP-2 and TRP-1, appear to be
specifically involved in melanogenesis. In addition, the activity
of these three enzymes has been described as being necessary for
the maximum activity of biosynthesis of eumelanins.
[0012] Head hair and body hair undergo a cycle. This cycle
comprises a growth phase (anagen phase), a degenerative phase
(catagen phase) and a rest phase (telogen phase) following which a
new anagen phase will develop. Due to this hair cycle, and unlike
the epidermal pigmentation unit, the follicular pigmentation unit
must also be cyclically renewed.
[0013] Canities (natural hair whitening) is linked to a specific
and gradual depletion of the hair melanocytes that affects both the
hair bulb melanocytes and the melanocyte precursor cells (Commo, et
al., Br. J. Dermatol., 2004, 150, 435-443). Other cell types
present in the haft follicles are not affected. In addition, this
depletion of melanocytes is not observed in the epidermis. The
cause of this gradual and specific depletion of melanocytes and
melanocyte precursors in the hair follicle has not been identified
to date.
[0014] It therefore appears necessary to combat the disappearance
of melanocytes from human hair follicles, a process that affects
both the active melanocytes of the bulbs and the quiescent
melanocytes of the upper region of the hair follicles, in order to
combat canities.
[0015] The assignee hereof has identified a means of combating hair
whitening by acting on the TRP-2 enzyme (WO 03/103568), especially
by increasing the level of GSH. Indeed, it has been demonstrated
that the expression of the TRP-2 enzyme is correlated with a higher
level of GSH in the melanocytes, the expression of TRP-2 induces an
increase in the level of GSH in the melanocytes. Thus, in the
melanocytes which do not express TRP-2 (for example, the melanocyte
precursors of hair), there is a low level of GSH in comparison with
the melanocytes that express the TRP-2 enzyme (for example, all the
skin melanocytes).
[0016] The assignee hereof has therefore identified a novel target
for the treatment of canities, more particularly it has
demonstrated that the compounds capable of increasing the level of
GSH in the melanocytes that are deficient in TRP-2 increase the
viability of these melanocytes, decrease hair whitening and lead,
unlike their depigmenting effect described in the literature, to
the restoring of hair pigmentation (FR 04/13756).
SUMMARY OF THE INVENTION
[0017] It has now been demonstrated that:
[0018] coumarin;
##STR00001##
and coumarin derivatives, especially 7-isopentenyloxycoumarin;
[0019] butylated hydroxyanisole (also denoted by
2-tert-butyl-4-hydroxyanisole and
3-tert-butyl-4-hydroxyanisole);
##STR00002##
[0020] and ethoxyquine (6-ethoxy-2,2,4-trimethyl-1H-quinoline, also
called ethoxytrimethyldihydroquinoline), by their ability to
increase the level of GSH in the melanocytes, counteract hair
whitening and effect the restoring of hair pigmentation.
[0021] Thus, the present invention features the administration of
at least one compound selected from coumarin and derivatives
thereof, butylated hydroxyanisole and ethoxyquine as an agent that
prevents, limits or stops the progression of canities, and
maintains and/or promotes the natural repigmentation of head hair
and/or body hair.
[0022] These compounds could also be administered as a mixture.
[0023] In particular, the present invention features the
administration of at least one compound selected from coumarin and
derivatives thereof, butylated hydroxyanisole and ethoxyquine and
mixtures thereof to prevent and/or limit and/or stop the
development of canities.
[0024] This invention also features the administration of at least
one compound selected from coumarin and derivatives thereof,
butylated hydroxyanisole and ethoxyquine for maintaining the
natural pigmentation of grey head hair and/or body hair.
[0025] The present invention also features compositions for
combating canities, comprising, formulated into a cosmetically
acceptable medium, at least one compound selected from coumarin and
derivatives thereof, butylated hydroxyanisole and ethoxyquine
combined with one other hair active agent selected from agents for
combating desquamative conditions of the scalp and/or plant
extracts with propigmenting activity.
[0026] This invention also features compositions for combating
canities comprising, formulated into a cosmetically acceptable
medium, at least one compound selected from coumarin and
derivatives thereof, butylated hydroxyanisole and ethoxyquine
combined with an agent that slows down hair loss or that promotes
its regrowth.
BRIEF DESCRIPTION OF THE DRAWINGS
[0027] FIG. 1 is a graph showing the effect of ethoxyquine on NHM:
measurement of the ROS induced by H.sub.2O.sub.2 and
[0028] FIG. 2 is a graph showing the effect of ethoxyquine on NHM:
measurement of the viability.
DETAILED DESCRIPTION OF BEST MODE AND SPECIFIC/PREFERRED
EMBODIMENTS OF THE INVENTION
[0029] The compositions according to the invention comprise an
amount of at least one compound selected from coumarin and
derivatives thereof, butylated hydroxyanisole and ethoxyquine of
from 0.001% to 10% by weight relative to the total weight of the
composition, preferentially from 0.01% to 5% by weight relative to
the total weight of the composition and even more preferentially
from 0.1% to 1% by weight relative to the total weight of the
composition.
[0030] The compositions according to the invention may be
administered orally or applied topically to the skin (over any
cutaneous area of the body covered with hair) and/or the scalp.
[0031] Orally, the compositions according to the invention may
contain the compound or compounds selected from coumarin and
derivatives thereof, butylated hydroxyanisole and ethoxyquine in
solution in a dietary liquid such as an optionally flavored aqueous
or aqueous-alcoholic solution. They may also be incorporated into
an ingestible solid excipient and may be, for example, in the form
of granules, pills, tablets or sugar-coated tablets. They may also
be dissolved in a dietary liquid that is itself optionally packaged
in ingestible capsules.
[0032] Depending on the method of administration, whether regime or
regimen, the compositions of the invention may be in any galenic
form normally used, particularly in cosmetology.
[0033] A preferred composition of the invention is a cosmetic
composition suitable for topical application to the scalp and/or
the skin.
[0034] For a topical application, the composition that can be
administered according to the invention may especially be in the
form of an aqueous, aqueous-alcoholic or oily solution or of a
dispersion of the lotion or serum type, of emulsions having a
liquid or semi-liquid consistency of the milk type, obtained by
dispersion of a fatty phase in an aqueous phase (O/W) or conversely
(W/O), or of suspensions or emulsions having a soft consistency of
the aqueous or anhydrous cream or gel type, or else of
microcapsules or microparticles, or of vesicular dispersions of
ionic and/or non-ionic type. It may thus be in the form of an
ointment, dye, cream, pomade, powder, patch, impregnated pad,
solution, emulsion or vesicular dispersion, lotion, gel, spray,
suspension, shampoo, aerosol or foam. They may be anhydrous or
aqueous. It may also consist of solid preparations that form soaps
or cleansing bars.
[0035] These compositions are formulated according to the usual
methods.
[0036] The composition that is administered according to the
invention may, in particular, be a composition for hair care, and
especially a shampoo, a setting lotion, a treating lotion, a
styling cream or gel, a dye composition (especially oxidation dye
compositions) optionally in the form of coloring shampoos,
restructuring lotions for the hair, or a mask.
[0037] The cosmetic composition according to the invention will
preferentially be a cream, hair lotion, shampoo or conditioner.
[0038] The amounts of the various constituents of the compositions
that are administered according to the invention are those
conventionally used in the fields in question.
[0039] When the composition according to the invention is an
emulsion, the proportion of the fatty phase may range from 5% to
80% by weight, and preferably from 5% to 50% by weight, relative to
the total weight of the composition. The oils, waxes, emulsifiers
and coemulsifiers included in the composition in the form of an
emulsion are selected from those conventionally used in the
cosmetics field. The emulsifier and coemulsifier are present in the
composition in an amount ranging from 0.3% to 30% by weight, and
preferably from 0.5% to 20% by weight, relative to the total weight
of the composition. The emulsion may, in addition, contain lipid
vesicles.
[0040] When the composition according to the invention is an oily
gel or solution, the fatty phase may represent more than 90% of the
total weight of the composition.
[0041] In one embodiment of the invention, the composition will be
such that the compound selected from coumarin and derivatives
thereof, butylated hydroxyanisole and ethoxyquine is encapsulated
in a coating such as microspheres, nanospheres, oleosomes or
nanocapsules.
[0042] This type of formulation proves advantageous because it
makes it possible to specifically target the hair follicle and thus
to release the active agent on its site of action.
[0043] By way of example, the microspheres can be prepared
according to the method described in EP-0,375,520.
[0044] The nanospheres can be in the form of an aqueous suspension
and be prepared according to the methods described in FR-0015686
and FR-0101438.
[0045] Oleosomes consist of an oil-in-water emulsion formed by oily
globules provided with a lamellar liquid crystal coating dispersed
in an aqueous phase (see EP-0,641,557 and EP-0,705,593).
[0046] The compound selected from coumarin and derivatives thereof,
butylated hydroxyanisole and ethoxyquine could also be encapsulated
in nanocapsules consisting of a lamellar coating obtained from a
silicone surfactant (see EP-0,780,115), the nanocapsules can also
be prepared based on water-dispersible sulfonic polyesters (see
FR-0113337).
[0047] The compound selected from coumarin and derivatives thereof,
butylated hydroxyanisole and ethoxyquine can also be complexed to
the surface of cationic oily globules, regardless of their size
(see EP-1,010,413, EP-1,010,414, EP-1,010,415, EP-1,010,416,
EP-1,013,338, EP-1,016,453, EP-1,018,363, EP-1,020,219,
EP-1,025,898, EP-1,120,101, EP-1,120,102, EP-1,129,684,
EP-1,160,005 and EP-1,172,077).
[0048] The compound selected from coumarin and derivatives thereof,
butylated hydroxyanisole and ethoxyquine may finally be complexed
to the surface of nanocapsules or nanoparticles provided with a
lamellar coating (see EP-0,447,318 and EP-0,557,489) and containing
a cationic surfactant at the surface (see the aforementioned
references for the cationic surfactants).
[0049] In particular, a composition will be preferred such that the
coating containing the compound selected from coumarin and
derivatives thereof, butylated hydroxyanisole and ethoxyquine has a
diameter of less than or equal to 10 .mu.m. When the coating does
not form a spherical vesicle, the diameter is understood to mean
the largest dimension of the vesicle.
[0050] In a known manner, the compositions according to the
invention may also contain adjuvants that are customary in the
cosmetics field, such as hydrophilic or lipophilic gelling agents,
hydrophilic or lipophilic additives, preservatives, antioxidants,
solvents, fragrances, fillers, screening agents, odor absorbers and
coloring materials. The amounts of these various adjuvants are
those conventionally used in the cosmetics field, and, for example,
are from 0.01% to 10% of the total weight of the composition. These
adjuvants, depending on their type, may be introduced into the
fatty phase, into the aqueous phase and/or into the lipid
spherules.
[0051] The compositions according to the invention may combine at
least one compound selected from coumarin and derivatives thereof,
butylated hydroxyanisole and ethoxyquine with other active agents.
Among these active agents, exemplary are:
[0052] agents modulating the differentiation and/or proliferation
and/or pigmentation of skin cells such as retinol and esters
thereof, vitamin D and derivatives thereof, oestrogens such as
oestradiol, cAMP modulators such as POMC derivatives, adenosine,
forskolin and derivatives thereof, prostaglandins and derivatives
thereof, triiodotrionine and derivatives thereof;
[0053] plant extracts such as those from Iridaceae or soya bean,
extracts which may or may not then contain isoflavones;
[0054] extracts from microorganisms;
[0055] free-radical scavengers such as .alpha.-tocopherol or esters
thereof, superoxide dismutases or the like, certain metal chelating
agents or ascorbic acid and esters thereof;
[0056] anti-seborrhoeic agents, such as certain sulfur-containing
amino acids, 13-cis-retinoic acid, cyproterone acetate;
[0057] other agents for combating the desquamative conditions of
the scalp such as zinc pyrithione, selenium disulfide, climbazole,
undecylenic acid, ketoconazole, piroctone olamine (octopirox) or
ciclopiroctone (ciclopirox);
[0058] in particular, they may be active agents that stimulate the
regrowth and/or that promote the slowing of hair loss, and more
particularly exemplary are:
[0059] nicotinic acid esters, especially including tocopheryl
nicotinate, benzyl nicotinate and C.sub.1-C.sub.6 alkyl nicotinates
such as methyl or hexyl nicotinates;
[0060] pyrimidine derivatives, such as
2,4-diamino-6-piperidinopyrimidine 3-oxide or "Minoxidil" described
in U.S. Pat. Nos. 4,139,619 and 4,596,812; Aminexil or
2,4-diaminopyrimidine 3-oxide described in WO 96/09048;
[0061] lipoxygenase-inhibiting agents or cyclooxidase-inducing
agents that promote hair regrowth such as those described by the
assignee hereof in EP-0,648,488;
[0062] anti-bacterial agents such as macrolides, pyranosides and
tetracyclines, and especially erythromycin;
[0063] calcium antagonists, such as cinnarizine, nimodipine and
nifedipine;
[0064] hormones, such as oestriol or the like, or thyroxine and
salts thereof;
[0065] anti-androgens, such as oxendolone, spironolactone,
diethylstilbestrol and flutamide;
[0066] steroid or non-steroid inhibitors of 5-.alpha.-reductases,
such as those described by the assignee hereof in EP-0,964,852 and
EP-1,068,858, or else finasteride;
[0067] ATP-dependent potassium channel agonists, such as
chromakalim and nicorandil; and
[0068] plant extracts with propigmenting activity, such as the
chrysanthemum extracts as described in FR-2768343 and Sanguisorba
extracts described in FR-2782920.
[0069] Preferably, the compound selected from coumarin and
derivatives thereof, butylated hydroxyanisole and ethoxyquine is
combined with at least one other hair active agent selected from
agents for combating desquamative conditions of the scalp, agents
that slow down hair loss or that promote its regrowth, plant
extracts with propigmenting activity.
[0070] The present invention also features a regime or regimen for
the cosmetic treatment of canities, wherein a composition as
defined previously comprising at least one compound selected from
coumarin and derivatives thereof, butylated hydroxyanisole and
ethoxyquine is administered or applied to the area to be
treated.
[0071] This invention also features a cosmetic treatment regime or
regimen useful to maintain the natural pigmentation of grey or
white head hair and/or body hair, wherein a composition as defined
previously comprising at least one compound selected from coumarin
and derivatives thereof, butylated hydroxyanisole and ethoxyquine
is administered or applied to the area to be treated.
[0072] The methods for treating canities and the pigmentation of
grey or white head hair and/or body hair may also entail ingesting
a composition comprising at least one compound selected from
coumarin and derivatives thereof, butylated hydroxyanisole and
ethoxyquine.
[0073] The areas to be treated may be, for example, and
non-limitingly, the scalp, eyebrows, moustache and/or beard and any
area of the skin covered with hair.
[0074] More particularly, the methods for the cosmetic treatment of
canities and the natural pigmentation of grey or white head hair
and/or body hair entails applying a composition comprising at least
one compound selected from coumarin and derivatives thereof,
butylated hydroxyanisole and ethoxyquine
[0075] The cosmetic treatment methods for combating canities and/or
for maintaining the natural pigmentation of grey or white head hair
and/or body hair may, for example, entail applying the composition
to the hair and scalp in the evening, keeping the composition on
overnight and optionally shampooing in the morning or washing the
hair using this composition and again leaving it in contact for a
few minutes before rinsing. The compositions according to the
invention have proved particularly advantageous when they are
applied in the form of an optionally rinse-out hair lotion or even
in the form of a shampoo.
[0076] In order to further illustrate the present invention and the
advantages thereof, the following specific examples are given, it
being understood that same are intended only as illustrative and in
nowise limitative. In said examples to follow, all parts and
percentages are given by weight, unless otherwise indicated.
EXAMPLE 1
Demonstration of the Activity of the Compounds of the Invention
[0077] 1-A-1. Protocol for Measuring the Reactive Oxygen Species
(ROS) Generated by an H.sub.2O.sub.2 Stress in Cultured Normal
Human Melanocytes (NHM):
[0078] The normal human melanocytes (NHMs) were inoculated at DO at
the density of 4.times.10.sup.4 cells/cm.sup.2. At D1, the culture
medium was replaced with the 10 .mu.M solution of
6-carboxy-2',7'-dichlorodihydrofluorescein diacetate,
di[acetoxymethyl ester] in PBS (H.sub.2DCFDA, C2938, Molecular
Probes). After 20 minutes, the H.sub.2DCFDA solution was replaced
with the culture medium. The NHMs were left for 30 minutes before
adding the H.sub.2O.sub.2 solution (250 .mu.M). The fluorescence
was measured after 15 minutes in a fluoroscan (excitation: 485 nm,
emission: 538 nm).
[0079] The compounds studied were used depending on their
properties (concentration, preincubation time). N-Acetylcysteine
(A9165-Sigma) was used as a reference molecule. The melanocytes
were pretreated, 12 h/18 h at 37.degree. C., with the compound
studied in the culture medium, before being brought into contact
for 20 minutes with H.sub.2DCFDA (10 .mu.M in PBS). The
H.sub.2DCFDA solution was then replaced with the culture medium
containing the active agent studied. After incubating for 30
minutes the oxidative stress was induced by addition of 250 .mu.M
of H.sub.2O.sub.2 in the culture medium. The fluorescence was
measured after 15 minutes in a fluoroscan (excitation: 485 nm,
emission: 538 nm).
[0080] 1-A-2. Results:
[0081] The results represent the crude fluorescence data, from
which the autofluorescence values of "blank" cells, expressed in
fluorescence units (fu), obtained during a representative
experiment, have been deducted.
[0082] The results are given in FIG. 1. A decrease of the reactive
oxygen species is indeed observed in the presence of
ethoxyquine.
[0083] 1-B-1. Protocol for Measuring the Viability (Toxicity
Control):
[0084] The normal human melanocytes (NHMs) were inoculated at DO at
the density of 4.times.10.sup.4 cells/cm.sup.2. After adhesion of
the cells (3 h), the compound studied was added to the culture
medium. After 24 h to 48 h, the cell viability was measured using
Alamar Blue (UP669413 UPTIMA, Interchim) according to the
instructions of the supplier.
[0085] 1-B-2. Results:
[0086] The results represent the fluorescent signal percentages
obtained for a representative experiment (measurement in
triplicate) (2 independent experiments were carried out) and
presented in the form of a % fluorescence curve as a function of
the concentration of the active agent studied (in .mu.M). The
results are given in FIG. 2.
EXAMPLE 2
Compositions
[0087] Hair Lotion:
TABLE-US-00001 courmarin 0.5 g propylene glycol 20 g 95.degree.
ethanol 30 g water qs for 100 g
[0088] This lotion was applied daily over the areas to be treated
and preferably over the entirety of the scalp for at least 10 days
and preferentially 1 to 2 months. A decrease in the appearance of
white or grey hairs and a repigmentation of the grey hairs was then
observed.
[0089] Treating Shampoo:
TABLE-US-00002 butylated hydroxyanisole 1.5 g polyglyceryl-3
hydroxyaryl ether 26 g hydroxy propyl cellulose marketed under the
2 g trademark KLUCELL G by Hercules preservatives qs 95.degree.
ethanol 50 g water qs for 100 g
[0090] This shampoo was used at each wash with an exposure time of
around one minute. A prolonged use, of around two months, led to
the slowing down of canities and to the gradual repigmentation of
grey hair.
[0091] This shampoo can also be used preventatively in order to
delay hair whitening.
[0092] Treating Gel:
TABLE-US-00003 ethoxyquine 0.75 g essential eucalyptus oils 1 g
econazole 0.2 g lauryl polyglyceryl-6 cetearyl glycol ether 1.9 g
preservatives qs CARBOPOL 934P marketed by BF Goodrich 0.3 g
Corporation neutralizing agent qs pH 7 water qs for 100 g
[0093] This gel was applied over the areas to be treated twice a
day (morning and evening) with a final massage. After applying for
three months, a repigmentation of the body hair or head hair of the
area treated was observed.
[0094] Flexible Gelatin Capsules:
TABLE-US-00004 coumarin 0.05 g/ capsule excipient qs
Three capsules can be taken per day.
[0095] Each patent, patent application, publication, text and
literature article/report cited or indicated herein is hereby
expressly incorporated by reference.
[0096] While the invention has been described in terms of various
specific and preferred embodiments, the skilled artisan will
appreciate that various modifications, substitutions, omissions,
and changes may be made without departing from the spirit thereof.
Accordingly, it is intended that the scope of the present invention
be limited solely by the scope of the following claims, including
equivalents thereof.
* * * * *